Synthesis and receptor binding of new thieno[2,3-d]pyrimidines as selective ligands of 5-HT3 receptors
With the aim to develop new potent and selective ligands of 5-HT3-type serotonin receptors and to acquire more information on their structure-affinity relationships, new thieno[2,3-d]pyrimidine derivatives 32-39 were synthesized and their binding to 5-HT3 versus 5-HT4 receptors was studied. Some of...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2008
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| Sorozat: | ARCHIV DER PHARMAZIE
341 No. 6 |
| doi: | 10.1002/ardp.200700205 |
| mtmt: | 1127905 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/16155 |
| Tartalmi kivonat: | With the aim to develop new potent and selective ligands of 5-HT3-type serotonin receptors and to acquire more information on their structure-affinity relationships, new thieno[2,3-d]pyrimidine derivatives 32-39 were synthesized and their binding to 5-HT3 versus 5-HT4 receptors was studied. Some of these new compounds exhibit good affinity for cortical 5-HT3 receptors, but not for 5-HT4 receptors. Among these derivatives, 6-ethyl-4-(4-methyl-l-piperazinyl)-2-(methylthio)thieno[2,3-d]pyrimidine 32 is the most potent ligand (K-i = 67 nM); it behaves as a competitive antagonist of the 5-HT3 receptor function in the guinea pig colon. Its binding interactions with 5-HT3A receptors were analysed by using receptor modelling and comparative docking. |
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| Terjedelem/Fizikai jellemzők: | 333-343 |
| ISSN: | 0365-6233 |